Acrizanib

SKU: orb1689897

Description

Acrizanib (LHA510) is a potent and selective VEGFR-2 tyrosine kinase inhibitor, demonstrating an IC50 of 17.4 nM in cellular assays. It is a valuable research tool for studying angiogenesis and has been utilized in both in vitro and in vivo models of cancer and other pathologies involving VEGF signaling.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1229453-99-9
• MW: 445.4
• Purity: 99.64% (May vary between batches)
• Formula: C₂₀H₁₈F₃N₇O₂
• SMILES: CNCc1cc(Oc2ccc3n(ccc3c2)C(=O)Nc2cc(n(C)n2)C(F)(F)F)ncn1
• Target: VEGFR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.49 mM);DMSO:37.8 mg/mL (84.87 mM)

Bioactivity

• Target IC50:
  VEGFR2:17.4 nM
• In Vivo:
  Rat ocular pharmacokinetic (PK) studies indicate that Acrizanib (compound 35) exhibits a notably different profile compared to compound 25, especially in terms of prolonged exposure within the posterior eye chamber (PEC). The area under the curve (AUC) ratio, reflecting Acrizanib's concentration in the PEC relative to its plasma levels, is significantly elevated, showing over 21000-fold higher exposure in the PEC compared to plasma by day 11. Additionally, Acrizanib demonstrates a substantially enhanced retina-to-plasma AUC exposure ratio after 10 days of administration (598× for Acrizanib versus 0.8× for compound 25), distinctively unlike compound 25.
• In Vitro:
  Acrizanib is a VEGFR-2 inhibitor with an IC50 of 17.4 nM for BaF3-KDR, and exhibits ≤10% remaining kinase activity against only 13 wild type kinases: CSF1R, Kit, PDGFRα, PDGFRβ, VEGFR1, VEGFR2, VEGFR3, Fms (soluble VEGFR1), DDR1, DDR2, TIE1, and ABL1 (nonphosphorylated) .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

LHA 510, LHA510, LHA-510, Acrizanib, VEGFR2

Compound Identifiers

PubChem CID

59394698